Biomedical Engineering Reference
In-Depth Information
Table 3.1  Experimental structures of complexes of GPCRs with different types of ligand
Receptor
Class/ a
subclass
Year
PDB code
Resolution (Å)
Ligand
Type b
Conformational state
Reference
Bovine rhodopsin
R/α
2000
1F88
2.8
11-cis retinal
Inverse agonist
Inactive
Palczewski et al. [ 26 ]
2004
1U19
2.2
11-cis retinal
Inverse agonist
Inactive
Okada et al. [ 78 ]
2011
3PQR
2.8
All-trans retinal
Agonist
Activated c
Choe et al. [ 35 ]
Squid rhodopsin
R/α
2008
2Z73
2.5
11-cis retinal
Inverse agonist
Inactive
Murakami and
Kouyama [ 79 ]
Human β2 adrenergic
R/α
2007
2RH1
2.4
Carazolol
Inverse agonist
Inactive
Rasmussen et al. [ 27 ]
2008
3D4S
2.8
Timolol
Inverse agonist
Inactive
Hanson et al. [ 80 ]
2010
3NY8
2.8
ICl118551
Inverse agonist
Inactive
Wacker et al. [ 81 ]
2010
3NYA
3.2
Alprenolol
Antagonist
Inactive
Wacker et al. [ 81 ]
2011
3P0G
3.5
BI-167107
Agonist
Activated d
Rasmussen et al. [ 29 ]
2011
3PDS
3.5
FAUC50
Irreversible
agonist
Intermediate
Rosenbaum et al. [ 82 ]
Activated e
2011
3SN6
3.2
BI-167107
Agonist
Rasmussen et al. [ 30 ]
Turkey β1 adrenergic R/α
2008
2VT4
2.7
Cyanopindolol
Antagonist
Inactive
Warne et al. [ 83 ]
2011
2Y00
2.5
Dobutamine
Partial agonist
Inactive
Warne et al. [ 84 ]
2011
2Y04
3.0
Salbutamol
Partial agonist
Inactive
Warne et al. [ 84 ]
2011
2Y02
2.6
Carmoterol
Agonist
Inactive
Warne et al. [ 84 ]
2011
2Y03
2.8
Isoprenaline
Agonist
Inactive
Warne et al. [ 84 ]
2011
2YCW
3.0
Carazolol
Inverse agonist
Inactive
Moukhametzianov
et al. [ 85 ]
2012
4AMI
3.2
Bucindolol
Biased agonist
Inactive
Warne et al. [ 76 ]
2012
4AMJ
2.3
Carvedilol
Biased agonist
Inactive
Warne et al. [ 76 ]
Human A2A adenosine R/α
2008
3EML
2.6
ZM241385
Inverse agonist
Inactive
Jaakola et al. [ 86 ]
2011
3QAK
2.7
UK-432097
Agonist
Intermediate
Xu et al. [ 87 ]
2011
2YDO
3.0
Adenosine
Agonist
Intermediate
Lebon et al. [ 88 ]
2011
2YDV
2.6
NECA
Agonist
Intermediate
Lebon et al. [ 88 ]
2011
3REY
3.3
XAC
Antagonist
Inactive
Dore et al. [ 89 ]
 
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